methylcobalamin

Small moleculeexperimental

Methylcobalamin (also known as mecobalamin, MeCbl, or MeB12) is one of the two forms of biologically active vitamin B12. Methyl-B12 is the principal form of circulating vitamin B12, hence the form, which is transported into peripheral tissue. Methylcobalamin is absorbed by the intestine by a specific mechanism, which uses the intrinsic factor, and by a diffusion process in which approximately 1% of the ingested dose is absorbed. Cyanocobalamin and hydroxycobalamin are forms of the vitamin that require conversion to methylcobalamin. Methylcobalamin alone or in combination with others compound are used to treat different diseases. Being a component of CEREFOLIN NAC it is used to treat Alzheimer's dementia. As a part of METANX® tablets is used for the dietary management of endothelial dysfunction in patients with diabetic peripheral neuropathy. Methylcobalamin exerted therapeutic effects on neuropathic pain in diabetics, possibly through its neurosynthesis and neuroprotective actions. The possible mechanisms can be considered as follows. (1) Methylcobalamin improved nerve conduction velocity; (2) methylcobalamin promoted injured nerve regeneration, recovering the neuromuscular functions in peripheral hyperalgesia and allodynia; and (3) methylcobalamin inhibited the ectopic spontaneous discharges from peripheral primary sensory neurons in neuropathic pain states. Methylcobalamin is the only form that can cross the blood-brain barrier and so can directly protect brain cells from degeneration. While crossing the barrier, it also stimulates production of serotonin, a chemical neurotransmitter responsible for elevated mood; research where Alzheimer’s patients were administered methylcobalamin showcased improvements in memory, communication skills, and emotions. It also helps form the myelin sheath, the insular coating around nerve cells that allow for electrical impulses to travel through the nervous system more efficiently. — NCATS

Clinical trial activity

22 trials · 41 clinical orgs · 0 marketing orgs

Phase 1
2
Phase 2
6
Phase 3
4
Phase 4
1

Earliest trial started Apr 1, 2008 (NCT00710359)

Timeline

2010s

  1. Jan 1, 2010

    Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 2017

    Earliest Phase 3 Sponsor(trial)

  3. Jan 1, 2018

    Earliest Phase 1 Sponsor(trial)

Indications

Approved for

Mechanism of action

  • UnclearSupplementation

    Unclear supplementation

Chemistry & pharmacology

Loading structure…

SMILES

[CH3-].[Co+3].C[C@@H](CNC(=O)CC[C@]1(C)[C@@H](CC(N)=O)[C@H]2[N-]C1=C(C)C3=NC(=CC4=NC(=C(C)C5=N[C@]2(C)[C@@](C)(CC(N)=O)[C@@H]5CCC(N)=O)[C@@](C)(CC(N)=O)[C@@H]4CCC(N)=O)C(C)(C)[C@@H]3CCC(N)=O)OP([O-])(=O)O[C@@H]6[C@@H](CO)O[C@@H]([C@@H]6O)N7C=NC8=C7C=C(C)C(C)=C8
Mol. weight
1344.3823 g/mol

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • adenosylcobalamin
  • cobalamin coenzyme
  • cobamamide
  • cobamamide
  • cobamamide
  • methyl b12
  • methyl b12
  • vitamin b12 coenzyme

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06990854N/AJul 1, 2025Hangzhou Third Hospital, Zhejiang Chinese Medical University
NCT05785585N/ASep 9, 2023Eurecat, Laboratorio Echevarne
NCT05751187Phase 2Jun 27, 2023Jiao Tong University, Merck
NCT05807711Phase 4Apr 1, 2023Alexandria University
NCT04786964Phase 3Sep 30, 2021Fortress Biotech
NCT04265534Phase 2Apr 30, 2020Calithera Biosciences
NCT03898336N/AJul 1, 2019Radboud University, University of Groningen, University of Heidelberg
NCT03885882Phase 1Apr 13, 2019Eisai
NCT03783104N/AFeb 1, 2019Paropakar Maternity and Women's Hospital, Sitaram Bhartia Institute of Science and Research, University of London
NCT03485404N/ASep 30, 2018Anhui Medical University, Huazhong University of Science and Technology, Jiao Tong University, Nanjing University, People's Liberation Army of China, Shaanxi Provincial People's Hospital, Xijing Hospital
NCT03626922Phase 1Aug 31, 2018Eli Lilly, Merck, NSABP Foundation
NCT03406793N/AFeb 20, 2018International Center for Diarrheal Disease Research, Johns Hopkins University, University of California, San Francisco, University of Colorado, Denver
NCT04706377N/AFeb 1, 2018Aristotle University of Thessaloniki, Sheffield Hallam University, University of Tuebingen
NCT03825042N/AJan 23, 2018Menarini Group
NCT04372316Phase 2Dec 25, 2017Peking University
NCT03909789N/ANov 17, 2017Los Angeles Biomedical Research Institute
NCT03548311Phase 3Nov 1, 2017Eisai, University of Tokushima
NCT03950674Phase 3Aug 7, 2017Merck
NCT01661309N/AMar 31, 2012University of West London
NCT01039792Phase 2/Phase 3 (Phase 3)Jan 1, 2010University of Arkansas, University of California, Davis, University of California, San Francisco
Showing 20 of 22 trials
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Organizations

Research & Development (41)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
MerckFor profit3132017
EisaiFor profit2122017
Foundation to Promote Research into Functional Vitamin B12 Deficiency, Bergen, NorwayAcademic/Hospital2012008
Jiao Tong UniversityAcademic/Hospital2122018
University Hospital of North NorwayAcademic/Hospital2012008
University of BergenAcademic/Hospital2212008
University of California, San FranciscoAcademic/Hospital2222010
Alexandria UniversityAcademic/Hospital1112023
Anhui Medical UniversityAcademic/Hospital1012018
Aristotle University of ThessalonikiAcademic/Hospital1112018
Calithera BiosciencesFor profit1112020
Eli LillyFor profit1012018
EurecatFor profit1112023
Fortress BiotechFor profit1112021
Hangzhou Third HospitalAcademic/Hospital1012025
Huazhong University of Science and TechnologyAcademic/Hospital1012018
International Center for Diarrheal Disease ResearchAcademic/Hospital1012018
Johns Hopkins UniversityAcademic/Hospital1012018
Laboratorio EchevarneFor profit1012023
Los Angeles Biomedical Research InstituteAcademic/Hospital1112017
41 organizations
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